PROTACs in Cancer Therapy: Targeted Degradation of GPX4, PARP, and Epigenetic Regulators
March 2026
in “
Journal of Enzyme Inhibition and Medicinal Chemistry
”
The review discusses the use of proteolysis targeting chimaeras (PROTACs) in cancer therapy, focusing on their ability to degrade specific proteins such as poly ADP-ribose polymerases (PARPs), glutathione peroxidase 4 (GPX4), and epigenetic regulators. PROTACs utilize the ubiquitin proteasome system to target and degrade overexpressed proteins, offering a promising alternative to traditional small-molecule drugs. The review highlights the design and synthetic strategies that have advanced PROTACs in cancer treatment and addresses challenges in their development, including target diversification, oral bioavailability, stability, degradation efficiency, and optimizing multivalent binding.